MK-801 的全身性给药可预防 N-甲基-D-天冬氨酸诱导的大鼠脑神经元变性。

Systemic administration of MK-801 prevents N-methyl-D-aspartate-induced neuronal degeneration in rat brain.

作者信息

Foster A C, Gill R, Kemp J A, Woodruff G N

出版信息

Neurosci Lett. 1987 May 19;76(3):307-11. doi: 10.1016/0304-3940(87)90420-4.

Abstract

MK-801 is a novel, potent and selective non-competitive antagonist of the N-methyl-D-aspartate (NMDA) subtype of excitatory amino acid receptors. Pretreatment of rats with MK-801 (1-10 mg/kg, i.p.) prevented neuronal degeneration in the hippocampus and striatum caused by direct intracranial injections of NMDA (20-120 nmol), but did not protect against the loss of neurones induced by kainate (2.5 nmol) injected into the striatum. Thus, MK-801 is a selective antagonist of neuronal degeneration caused by excessive stimulation of NMDA receptors in vivo.

摘要

MK-801是一种新型、强效且具有选择性的兴奋性氨基酸受体N-甲基-D-天冬氨酸（NMDA）亚型非竞争性拮抗剂。用MK-801（1 - 10毫克/千克，腹腔注射）对大鼠进行预处理，可预防因直接颅内注射NMDA（20 - 120纳摩尔）导致的海马体和纹状体神经元变性，但不能防止向纹状体注射海藻酸（2.5纳摩尔）引起的神经元丢失。因此，MK-801是体内NMDA受体过度刺激所致神经元变性的选择性拮抗剂。